（11）C]Cimbi-36 标记的 5-羟色胺 2A 受体激动剂在人脑中的结合：测试-重测再现性和与拮抗剂（18）F]altanserin 的对头比较。
Serotonin 2A receptor agonist binding in the human brain with [(11)C]Cimbi-36: Test-retest reproducibility and head-to-head comparison with the antagonist [(18)F]altanserin.
机构信息
Neurobiology Research Unit, Center for Integrated Molecular Brain Imaging (Cimbi), Copenhagen University Hospital, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark.
Neurobiology Research Unit, Center for Integrated Molecular Brain Imaging (Cimbi), Copenhagen University Hospital, Rigshospitalet, Blegdamsvej 9, 2100 Copenhagen, Denmark; Faculty of Health and Medical Sciences, University of Copenhagen, Denmark.
出版信息
Neuroimage. 2016 Apr 15;130:167-174. doi: 10.1016/j.neuroimage.2016.02.001. Epub 2016 Feb 11.
INTRODUCTION
[(11)C]Cimbi-36 is a recently developed serotonin 2A (5-HT2A) receptor agonist positron emission tomography (PET) radioligand that has been successfully applied for human neuroimaging. Here, we investigate the test-retest variability of cerebral [(11)C]Cimbi-36 PET and compare [(11)C]Cimbi-36 and the 5-HT2A receptor antagonist [(18)F]altanserin.
METHODS
Sixteen healthy volunteers (mean age 23.9 ± 6.4years, 6 males) were scanned twice with a high resolution research tomography PET scanner. All subjects were scanned after a bolus of [(11)C]Cimbi-36; eight were scanned twice to determine test-retest variability in [(11)C]Cimbi-36 binding measures, and another eight were scanned after a bolus plus constant infusion with [(18)F]altanserin. Regional differences in the brain distribution of [(11)C]Cimbi-36 and [(18)F]altanserin were assessed with a correlation of regional binding measures and with voxel-based analysis.
RESULTS
Test-retest variability of [(11)C]Cimbi-36 non-displaceable binding potential (BPND) was consistently <5% in high-binding regions and lower for reference tissue models as compared to a 2-tissue compartment model. We found a highly significant correlation between regional BPNDs measured with [(11)C]Cimbi-36 and [(18)F]altanserin (mean Pearson's r: 0.95 ± 0.04) suggesting similar cortical binding of the radioligands. Relatively higher binding with [(11)C]Cimbi-36 as compared to [(18)F]altanserin was found in the choroid plexus and hippocampus in the human brain.
CONCLUSIONS
Excellent test-retest reproducibility highlights the potential of [(11)C]Cimbi-36 for PET imaging of 5-HT2A receptor agonist binding in vivo. Our data suggest that Cimbi-36 and altanserin both bind to 5-HT2A receptors, but in regions with high 5-HT2C receptor density, choroid plexus and hippocampus, the [(11)C]Cimbi-36 binding likely represents binding to both 5-HT2A and 5-HT2C receptors.
简介
[(11)C]Cimbi-36 是一种新开发的血清素 2A（5-HT2A）受体激动剂正电子发射断层扫描（PET）示踪剂，已成功应用于人类神经影像学。在这里，我们研究了脑 [(11)C]Cimbi-36 PET 的测试-重测变异性，并比较了 [(11)C]Cimbi-36 和 5-HT2A 受体拮抗剂 [(18)F]altanserin。
方法
16 名健康志愿者（平均年龄 23.9±6.4 岁，6 名男性）使用高分辨率研究型断层扫描 PET 扫描仪进行了两次扫描。所有受试者均在 [(11)C]Cimbi-36 静脉推注后进行扫描；8 名志愿者进行了两次扫描，以确定 [(11)C]Cimbi-36 结合指标的测试-重测变异性，另外 8 名志愿者在 [(18)F]altanserin 静脉推注后进行了一次扫描加恒速输注。用局部脑区 [(11)C]Cimbi-36 和 [(18)F]altanserin 分布的相关分析和基于体素的分析来评估脑区的差异。
结果
[(11)C]Cimbi-36 不可置换结合潜能（BPND）的测试-重测变异性在高结合区始终<5%，且参考组织模型比 2 组织室模型低。我们发现，用 [(11)C]Cimbi-36 和 [(18)F]altanserin 测量的局部 BPND 之间存在高度显著的相关性（平均 Pearson's r：0.95±0.04），这表明放射性配体的皮质结合相似。与 [(18)F]altanserin 相比，[(11)C]Cimbi-36 在人类大脑的脉络丛和海马体中发现相对较高的结合。
结论
出色的测试-重测可重复性突出了 [(11)C]Cimbi-36 在体内成像 5-HT2A 受体激动剂结合方面的潜力。我们的数据表明，Cimbi-36 和 altanserin 都与 5-HT2A 受体结合，但在 5-HT2C 受体密度较高的区域，脉络丛和海马体，[(11)C]Cimbi-36 结合可能代表与 5-HT2A 和 5-HT2C 受体的结合。
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